Table S1-S7 from Antibody–Exatecan Conjugates with a Novel Self-immolative Moiety Overcome Resistance in Colon and Lung Cancer

Supplementary Table S1 shows cytotoxicity of exatecan compared to DXd. Supplementary Table S2 shows selected hematologic parameters and biochemical parameters from the repeat-dose administration of exatecan mesylate studies in rats. Supplementary Table S3 shows in vitro ADC stability study of total antibody, ADC and free payload. Supplementary Table S4 shows pharmacokinetic parameters of total antibody, ADC and free payload. Supplementary Table S5 shows ADC (T: T-1000-e; D: DS-8201a) internalization rate on cell lines with different HER2 expression level. Supplementary Table S6 shows correlation of exatecan release and target expression. Supplementary Table S7 shows In vitro cytotoxicicity of HER-targeting MTX-1000, TROP2 targeting MTX-132 and HER3-targeting Patritumab-T1000-exatecan and their counterpart DXd-ADC.

补充表 S1 展示了与 DXd 相较之下，exatecan 的细胞毒性。补充表 S2 展示了重复剂量给药的 exatecan 甲磺酸酯研究中小鼠选择的血液学参数和生化参数。补充表 S3 展示了总抗体、抗体药物偶联物（ADC）和游离有效载荷的体外 ADC 稳定性研究。补充表 S4 展示了总抗体、ADC 和游离有效载荷的药代动力学参数。补充表 S5 展示了具有不同 HER2 表达水平的细胞系上 ADC（T：T-1000-e；D：DS-8201a）的内化率。补充表 S6 展示了 exatecan 释放与靶点表达的相关性。补充表 S7 展示了针对 HER 的 MTX-1000、TROP2 靶向的 MTX-132、HER3 靶向的 Patritumab-T1000-exatecan 及其对应物 DXd-ADC 的体外细胞毒性。